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The invertebrate pharmacology of insecticides acting at nicotinic acetylcholine receptors

机译:对烟碱型乙酰胆碱受体起作用的杀虫剂的无脊椎动物药理作用

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The nicotinic acetylcholine receptor (nAChR) is a ligand-gated ion channel composed of 5 protein subunits arranged around a central cation selective pore. Several classes of natural and synthetic insecticides mediate their effect through interacting at nAChRs. This review examines the basic pharmacology of the neonicotinoids and related chemistry, with an emphasis on sap-feeding insects from the order Hemiptera, the principle pest target for such insecticides. Although the receptor subunit stoichiometry for endogenous invertebrate nAChRs is unknown, there is clear evidence for the existence of distinct neonicotinoid binding sites in native insect preparations, which reflects the predicted wide repertoire of nAChRs and differing pharmacology within this insecticide class. The spinosyns are principally used to control chewing pests such as Lepidoptera, whilst nereistoxin analogues are used on pests of rice and vegetables through contact and systemic action, the pharmacology of both these insecticides is unique and different to that of the neonicotinoids.
机译:烟碱型乙酰胆碱受体(nAChR)是一个配体门控离子通道,由围绕中央阳离子选择性孔排列的5个蛋白亚基组成。几类天然和合成杀虫剂通过与nAChRs相互作用来介导其作用。这篇综述研究了新烟碱类药物的基本药理学和相关化学,重点研究了半翅目(Hemiptera)的树液喂养昆虫,该昆虫是这类杀虫剂的主要害虫目标。尽管内源性无脊椎动物nAChRs的受体亚基化学计量是未知的,但有明显的证据表明天然昆虫制剂中存在不同的新烟碱类结合位点,这反映了nAChRs的预计成分广泛,并且在该杀虫剂类别中具有不同的药理作用。刺糖多孢菌素主要用于控制咀嚼害虫,例如鳞翅目,而神经毒素类似物通过接触和全身作用用于水稻和蔬菜的害虫,这两种杀虫剂的药理作用是独特的,与新烟碱类药物不同。

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